发明名称 CRF antagonistic quino- and quinazolines
摘要 This invention concerns compounds of formula including the stereoisomers and the pharmaceutically acceptable acid addition salt forms thereof, wherein R<1 >is C1-6alkyl, NR<6>R<7>, OR<6 >or SR<7>; R<2 >is hydrogen, C1-6alkyl, C1-6alkyloxy or C1-6alkylthio; R<3 >is Ar<1 >or Het<1>; R<4 >and R<5 >are each independently selected from hydrogen, halo, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, cyano, nitro, amino, and mono- or di(C1-6alkyl)amino; R<6 >is hydrogen, C1-6alkyl, C1-6alkylsulfonyl, C1-6alkylsulfoxy or C1-6alkylthio; R<7 >is hydrogen, C1-8alkyl, mono- or di(C3-6cyclo-alkyl)methyl, C3-6cycloalkyl, C3-6alkenyl, hydroxyC1-6alkyl, C1-6alkylcarbonyloxy-C1-6alkyl or C1-6alkyloxyC1-6alkyl; R<6 >is C1-8alkyl, mono- or di(C3-6cycloalkyl)-methyl, Ar<2>CH2, C1-6alkyloxyC1-6alkyl, hydroxyC1-6alkyl, C3-6alkenyl, thienylmethyl, furanylmethyl, C1-6alkylthioC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)amino, C1-6alkylcarbonylC1-6alkyl; or R<6 >and R<7 >taken together with the nitrogen atom to which they are attached may form a pyrrolidinyl, piperidinyl, homopiperidinyl or morpholinyl group, optionally substituted with C1-6alkyl or C1-6alkyloxyC1-6alkyl; and Ar<1 >and Ar<2 >are each optionally substituted phenyl; and Het<1 >is optionally substituted pyridinyl; having CRF receptor antagonistic properties; pharmaceutical compositions containing such compounds as active ingredients; methods of trea
申请公布号 US2004121998(A1) 申请公布日期 2004.06.24
申请号 US20030648843 申请日期 2003.08.26
申请人 NEUROCRINE BIOSCIENCES, INC. 发明人 HUANG CHARLES;WILCOXEN KEITH M.;CHEN CHEN;HADDACH MUSTAPHA;MCCARTHY JAMES R.
分类号 A61K31/47;A61K31/4709;A61K31/517;A61P1/00;A61P25/00;A61P25/08;A61P25/22;A61P25/24;A61P43/00;C07D215/12;C07D215/22;C07D215/233;C07D215/36;C07D215/42;C07D239/94;C07D401/04;(IPC1-7):A61K31/55;A61K31/537;A61K31/470 主分类号 A61K31/47
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